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Description
An understanding of pharmacokinetics is necessary to ensure that drugs that are active in vitro will also be active in the human body. The optimization of the pharmacokinetic properties of lead compounds is therefore of central importance to drug development.

In this new edition of a bestseller, all the contents have been updated and new material has been added, especially in the areas of toxicity testing and high throughput analysis. The authors, all of them employed at Pfizer in the discovery and development of new active substances, discuss the significant parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. They cover everything from the fundamental principles right up to the impact of pharmacokinetic parameters on the discovery of new drugs.

From the contents:
  • Physicochemistry
  • Pharmacokinetics
  • Absorption
  • Distribution
  • Clearance
  • Renal Clearance
  • Metabolic (Hepatic) Clearance
  • Toxicity
  • Inter-Species Scaling
  • High(er) Throughput ADME Studies

While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the clear and accessible style makes this book equally suitable for teaching students of pharmacy and related subjects, especially for those who feel that pharmacokinetics is covered too briefly in the standard textbooks.

About the Author
Dennis Smith has worked in the pharmaceutical industry for the past 30 years since gaining his Ph.D. from the University of Manchester. For the last 18 years he has been at Pfizer global research and Development, Sandwich where he is vice President-Pharmacokinetics, Dynamics and Metabolism. His research interests and publications span all aspects of Drug Discovery and Development particularly where drug metabolism knowledge can impact on the design of more efficacious and safer drugs. During this 30-year span he has helped in the Discovery and Development of eight marketed NCEs, with hopefully several more to come. He has authored over 100 publications. He is active in a teaching role holding appointments as visiting Professor at the University of Liverpool and Honorary Senior Lecturer at the University of Aberdeen and lectures widely to students at several other Universities.
His wish in much of his work is "to inspire another generation to take up the cudgel against disease".

Han van de Waterbeemd studied physical organic chemistry at the Technical University of Eindhoven and did a Ph.D. in medicinal chemistry at the University of Leiden, The Netherlands. After a post-doc with Bernard Testa at the University of Lausanne, Switzerland, he became a faculty member for 5 years and taught medicinal chemistry to pharmacy students at the universities of Berne and Basel, Switzerland. In his pharmaceutical career he worked for Roche, Pfizer and Astra-Zeneca where he is now global project leader of their platform for in silico predictions of ADME/Tax properties. He published more than 133 peer reviewed papers and book chapters, and (co-) edited 11 books. His research interests include the role of physicochemical and structural molecular properties in drug disposition and in silico modeling of ADMET properties.

Don Walker has a degree in Biochemistry from the University of London and spent four years assisting research involving the biochemistry of inborn errors of metabolism. He joined the Drug Metabolism Department at Pfizer in Sandwich in 1986 and since then has contributed to the drug metabolism and pharmacokinetic evaluations on several drug discovery and development projects including amlodopine, dofetilide, sildenafil, variconazole and maraviroc. He has published numerous papers on drug metabolism and pharmacokinetics and during his career at Pfizer he has been an active contributor to the UK Drug Metabolism Discussion Group, at various times having served as committee member, chairman and course tutor.

New to Edition
The second edition features several new subchapters on novel aspects or on fields that have received fresh attention by pharmaceutical scientists.
In the Physiochemistry chapter, new sections on compound solubility and ionisation have been added. Toxicity testing in animals has been expanded to cover single animal studies, and the recently evolved concept of ADME space is now introduced in the section on high throughput studies, where most of the subchapters have been rewritten and expanded.
Data in figures and tables have been updated where appropriate, and new references have been added.